The effect of orlistat and ezetimibe, alone or in combination, on serum LDL and small dense LDL cholesterol levels in overweight and obese patients with hypercholesterolaemia

<p>
Background:
Increased concentrations of low density lipoprotein cholesterol (LDL-C), as well as of small dense LDL-C (sdLDL-C), are considered as cardiovascular risk factors.
</p>
<p>Objective: An assessment of the effects of ezetimibe and orlistat administration, alone or in combination, on LDL-C and sdLDL-C levels (primary endpoint), as well as on anthropometric variables and metabolic parameters (secondary endpoints) in overweight and obese patients [body mass index (BMI) &gt; 28 kg/m2] with hypercholesterolaemia [total cholesterol &gt; 200 mg/dL (5.2 mmol/L)].</p>
<p>Methods: Eighty six subjects were prescribed a low-fat low-calorie diet and were randomly allocated to receive orlistat 120 mg, 3 times daily (O group), ezetimibe 10 mg/day (E group) or both (OE group) for 6 months.</p>
<p>Results: Significant reductions in LDL-C (−19%, −21%, −32% in groups O, E and OE, respectively, all p &lt; 0.01 vs. baseline) and sdLDL-C levels (−45%, −48%, −76% in groups O, E, OE, respectively, all p &lt; 0.01 vs. baseline) were observed. Group OE experienced a significantly greater reduction in LDL-C and sdLDL-C levels compared with groups O and E (p &lt; 0.05). Furthermore, significant reductions of BMI, homeostasis model assessment (HOMA) index, serum uric acid, transaminase activities and plasma lipoprotein-associated phospholipase A2 (Lp-PLA2) activity were observed in the O and OE groups. Gamma-glutamyl transpeptidase activity and Lp-PLA2 activity improved significantly more with the combination treatment compared with either orlistat or ezetimibe monotherapy.</p>
<p>Conclusions: Orlistat and ezetimibe combination had a more favorable effect on LDL-C and sdLDL-C levels in overweight and obese hypercholesterolaemic patients than either drug alone. Furthermore, orlistat, alone or in combination with ezetimibe, additionally improved several anthropometric and metabolic variables.</p>
<p></p>
<p><strong>Current Medical Research and Opinion, 2008, Vol. 24, No. 7, Pages 1919-1929 </strong></p>